EP2084165A4 - Positiv geladene, wasserlösliche prodrugs von oxicamen und verwandten verbindungen mit sehr hoher hautpenetrationsrate - Google Patents
Positiv geladene, wasserlösliche prodrugs von oxicamen und verwandten verbindungen mit sehr hoher hautpenetrationsrateInfo
- Publication number
- EP2084165A4 EP2084165A4 EP06809572A EP06809572A EP2084165A4 EP 2084165 A4 EP2084165 A4 EP 2084165A4 EP 06809572 A EP06809572 A EP 06809572A EP 06809572 A EP06809572 A EP 06809572A EP 2084165 A4 EP2084165 A4 EP 2084165A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- oxicams
- positively charged
- related compounds
- skin penetration
- penetration rate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2006/053741 WO2008044095A1 (en) | 2006-10-11 | 2006-10-11 | Positively charged water-soluble prodrugs of oxicams and related compounds with very high skin penetration rate |
Publications (3)
Publication Number | Publication Date |
---|---|
EP2084165A1 EP2084165A1 (de) | 2009-08-05 |
EP2084165A4 true EP2084165A4 (de) | 2011-01-05 |
EP2084165B1 EP2084165B1 (de) | 2013-06-12 |
Family
ID=39282470
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP06809572.8A Not-in-force EP2084165B1 (de) | 2006-10-11 | 2006-10-11 | Positiv geladene, wasserlösliche prodrugs von oxicamen und verwandten verbindungen mit sehr hoher hautpenetrationsrate |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP2084165B1 (de) |
JP (1) | JP5378221B2 (de) |
CN (1) | CN101522692A (de) |
WO (1) | WO2008044095A1 (de) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20090221703A1 (en) | 2006-07-09 | 2009-09-03 | Chongxi Yu | High penetration composition and uses thereof |
US20090238763A1 (en) | 2006-07-09 | 2009-09-24 | Chongxi Yu | High penetration compositions and uses thereof |
JP5378219B2 (ja) | 2006-10-02 | 2013-12-25 | テックフィールズ バイオケム カンパニー リミテッド | 非常に高い皮膚浸透率を有するプロスタグランジン及び関連化合物の正荷電水溶性プロドラッグ |
JP5424887B2 (ja) | 2006-11-08 | 2014-02-26 | チョンシー ユー | ペプチド及び関連化合物の経皮送達システム |
CA2671938C (en) | 2006-12-10 | 2017-10-17 | Chongxi Yu | Transdermal delivery systems of beta-lactam antibiotics |
CN101605754B (zh) | 2007-01-15 | 2015-09-16 | 于崇曦 | 具有快速皮肤穿透速度的带正电荷的水溶性的维生素a酸类和类维生素a酸化合物的前药 |
ES2607901T3 (es) | 2007-01-31 | 2017-04-04 | Chongxi Yu | Profármacos hidrosolubles cargados positivamente de 1H-imidazo[4,5-c]quinolin-4-aminas y compuestos relacionados con ratas de penetración de piel muy altas |
KR101853971B1 (ko) * | 2007-06-04 | 2018-05-02 | 테크필즈 인크 | 매우 높은 피부 및 막 침투율을 가지는 비스테로이드성 소염제(nsaia) 약물전구체 및 이들의 새로운 의약적 용도 |
KR20210123406A (ko) * | 2008-12-04 | 2021-10-13 | 충시 위 | 고투과력을 가진 조성물 및 이의 적용 |
ES2845612T3 (es) | 2009-05-08 | 2021-07-27 | Techfields Biochem Co Ltd | Composiciones de profármaco de alta penetración de péptidos y compuestos relacionados con péptidos |
US9969751B2 (en) | 2009-06-10 | 2018-05-15 | Techfields Pharma Co., Ltd. | High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds |
PL2849738T3 (pl) | 2012-01-18 | 2024-05-13 | Techfields Pharma Co., Ltd. | Kompozycje proleków o dużej szybkości przenikania i ich kompozycje farmaceutyczne do leczenia chorób płuc |
CA2917145C (en) | 2013-03-15 | 2023-10-24 | Techfields Pharma Co., Ltd. | Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases |
US20160168108A1 (en) | 2014-12-16 | 2016-06-16 | Adt Pharmaceuticals, Inc. | Method of treating or preventing ras-mediated diseases |
US9862698B2 (en) | 2014-12-16 | 2018-01-09 | Adt Pharmaceuticals, Inc. | Indenyl compounds, pharmaceutical compositions, and medical uses thereof |
CN106632403B (zh) * | 2017-01-23 | 2018-09-11 | 牡丹江医学院 | 一种手术用止痛消炎药及其制备方法 |
EP3784228A1 (de) | 2018-04-26 | 2021-03-03 | ADT Pharmaceuticals, LLC | Antikrebs-indene, indane, azaindene, azodiindane, pharmazeutische zusammensetzungen und verwendungen |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0208404A2 (de) * | 1985-05-29 | 1987-01-14 | Pfizer Inc. | Benzothiazindioxydderivate |
US20040254182A1 (en) * | 2000-01-28 | 2004-12-16 | Mulvihill Mark Joseph | Enhanced propertied pharmaceuticals |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3787324A (en) | 1971-03-01 | 1974-01-22 | Warner Lambert Co | 4-hydroxy-3-(3-isoxazolocarbamyl)-2h-1,2-benzothiazine 1,dioxides and process for their production |
US3704298A (en) * | 1971-06-22 | 1972-11-28 | Warner Lambert Co | 4-acyloxy-3-(2-isoxazolocarbamyl)-2h-1,2-benzothiazine 1,1-dioxides |
AU518216B2 (en) | 1977-09-06 | 1981-09-17 | Hafslund Nycomed Pharma Aktiengesellschaft | Thienothiazine derivatives |
JPS5714589A (en) | 1980-06-27 | 1982-01-25 | Mitsui Toatsu Chem Inc | Benzothiazine derivative, its preparation and drug composition |
IN162323B (de) * | 1983-12-21 | 1988-04-30 | Pfizer | |
US4551452A (en) * | 1983-12-21 | 1985-11-05 | Pfizer Inc. | Anti-inflammatory 2-methyl-2H-1,2-benzo-(or -thieno-)thiazine-3-carboxamide 1,1-dioxide derivatives, compositions, and method of use therefor |
JPS60184077A (ja) * | 1984-02-23 | 1985-09-19 | フアイザー・インコーポレーテツド | 抗炎症性オキシム前駆薬 |
WO1989003682A1 (en) * | 1987-10-26 | 1989-05-05 | Pfizer Inc. | Benzothiazine dioxide derivatives |
MY106598A (en) * | 1988-08-31 | 1995-06-30 | Australian Commercial Res & Development Ltd | Compositions and methods for drug delivery and chromatography. |
US5607691A (en) | 1992-06-12 | 1997-03-04 | Affymax Technologies N.V. | Compositions and methods for enhanced drug delivery |
AU4534593A (en) * | 1992-06-12 | 1994-01-04 | Affymax Technologies N.V. | Compositions and methods for enhanced drug delivery |
US5654337A (en) | 1995-03-24 | 1997-08-05 | II William Scott Snyder | Topical formulation for local delivery of a pharmaceutically active agent |
AUPN531195A0 (en) | 1995-09-11 | 1995-10-05 | J.W. Broadbent Nominees Pty. Ltd. | Lipid extract having anti-inflamatory activity |
KR100213465B1 (ko) | 1996-11-01 | 1999-08-02 | 최좌진 | 케토프로펜 패취 조성물 |
US5885597A (en) | 1997-10-01 | 1999-03-23 | Medical Research Industries,Inc. | Topical composition for the relief of pain |
MXPA00012844A (es) | 1998-07-07 | 2004-05-21 | Transdermal Technologies Inc | Composiciones para la liberacion transdermica rapida y sin irritacion de agentes farmaceuticamente activos y metodos para formular tales composiciones y liberar los mismos. |
US6416772B1 (en) | 2001-01-12 | 2002-07-09 | H. Wayne Van Engelen | Topical dermal anaesthetic |
US7052715B2 (en) | 2003-04-11 | 2006-05-30 | All Natural Fmg, Inc. | Alcohol-free transdermal analgesic composition and processes for manufacture and use thereof |
-
2006
- 2006-10-11 WO PCT/IB2006/053741 patent/WO2008044095A1/en active Search and Examination
- 2006-10-11 CN CN200680056073A patent/CN101522692A/zh active Pending
- 2006-10-11 JP JP2009531929A patent/JP5378221B2/ja not_active Expired - Fee Related
- 2006-10-11 EP EP06809572.8A patent/EP2084165B1/de not_active Not-in-force
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0208404A2 (de) * | 1985-05-29 | 1987-01-14 | Pfizer Inc. | Benzothiazindioxydderivate |
US20040254182A1 (en) * | 2000-01-28 | 2004-12-16 | Mulvihill Mark Joseph | Enhanced propertied pharmaceuticals |
Non-Patent Citations (5)
Title |
---|
GIRAUD I ET AL: "Application to a Cartilage Targeting Strategy: Synthesis and in Vivo Biodistribution of 14C-Labeled Quaternary Ammonium-Glucosamine Conjugates", BIOCONJUGATE CHEM., vol. 11, 17 February 2000 (2000-02-17), pages 212 - 218, XP002611626 * |
NICOLAS COLETTE ET AL: "New Quaternary Ammonium Oxicam Derivatives Targeted toward Cartilage: Synthesis, Pharmacokinetic Studies, and Antiinflammatory Potency", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 42, 1 January 1999 (1999-01-01), pages 5235 - 5240, XP002165071, ISSN: 0022-2623, DOI: 10.1021/JM991120O * |
See also references of WO2008044095A1 * |
SONG N ET AL: "Synthesis of a derivative quaternary ammonium-ibuprofen", JOURNAL OF OCEAN UNIVERSITY OF QINGDAO,, vol. 32, no. 6, 1 January 2002 (2002-01-01), pages 911 - 913, XP001539131 * |
VENUTI M C ET AL: "SYNTHESIS AND BIOLOGICAL EVALUATION OF OMEGA-(N,N,N-TRIALKYLAMMONIUM) ALKYL ESTERS AND THIOESTERS OF CARBOXYLIC ACID NONSTEROIDAL ANTIINFLAMMATORY AGENTS", PHARMACEUTICAL RESEARCH, KLUWER ACADEMIC PUBLISHERS, NEW YORK, NY, US, vol. 6, no. 10, 1 January 1989 (1989-01-01), pages 867 - 873, XP001098334, ISSN: 0724-8741, DOI: 10.1023/A:1015960522189 * |
Also Published As
Publication number | Publication date |
---|---|
JP2010505936A (ja) | 2010-02-25 |
EP2084165A1 (de) | 2009-08-05 |
EP2084165B1 (de) | 2013-06-12 |
JP5378221B2 (ja) | 2013-12-25 |
WO2008044095A1 (en) | 2008-04-17 |
CN101522692A (zh) | 2009-09-02 |
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A4 | Supplementary search report drawn up and despatched |
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